Page last updated: 2024-11-13

as 1842856

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Description

5-amino-7-(cyclohexylamino)-1-ethyl-6-fluoro-4-oxo-1,4-dihydroquinoline-3-carboxylic acid: inhibits Foxo1 transactivation; inhibits mRNA levels of glucose-6-phosphatase and phosphoenolpyruvate carboxykinase; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

AS1842856 : A quinolone that is 4-quinolone substituted at positions 1, 3, 5, 6 and 7 by ethyl, carboxy, amino, fluorine, and cyclohexylamino groups, respectively. It can directly bind to and block the transcription activity of the active forkhead box protein O1 (Foxo1), but not the Ser256-phosphorylated form. It induces cell death and growth arrest in Burkitt lymphoma cell lines at low concentrations. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Cross-References

ID SourceID
PubMed CID72193864
CHEMBL ID5192734
CHEBI ID145800
SCHEMBL ID17387387
MeSH IDM0552293

Synonyms (26)

Synonym
5-amino-7-(cyclohexylamino)-1-ethyl-6-fluoro-4-oxo-1,4-dihydroquinoline-3-carboxylic acid
5-amino-7-(cyclohexylamino)-1-ethyl-6-fluoro-1,4-dihydro-4-oxo-3-quinolinecarboxylic acid
foxo1 inhibitor
as 1842856
as1842856
as-1842856
CHEBI:145800
836620-48-5
S8222
SCHEMBL17387387
CS-6192
HY-100596
CHEMBL5192734 ,
5-amino-7-(cyclohexyl-amino)-1-ethyl-6-fluoro-4-oxo-1,4-dihydroquinoline-3-carboxylic acid
AKOS032945046
BCP17382
as-1842856;as 1842856
EX-A2538
BS-17713
CCG-267998
C76673
AC-36120
EN300-95548
5-amino-7-(cyclohexylamino)-1-ethyl-6-fluoro-4-oxoquinoline-3-carboxylic acid
Z1270398088
bdbm50600522

Research Excerpts

[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (6)

RoleDescription
hypoglycemic agentA drug which lowers the blood glucose level.
anti-obesity agentAny substance which is used to reduce or control weight.
autophagy inhibitorAny compound that inhibits the process of autophagy (the self-digestion of one or more components of a cell through the action of enzymes originating within the same cell).
antineoplastic agentA substance that inhibits or prevents the proliferation of neoplasms.
apoptosis inducerAny substance that induces the process of apoptosis (programmed cell death) in multi-celled organisms.
forkhead box protein O1 inhibitorAny inhibitor that acts on forkhead box protein O1 (FOXO1).
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Drug Classes (6)

ClassDescription
quinolinemonocarboxylic acidAny aromatic carboxylic acid that contains a quinoline moiety that is substituted by one carboxy substituent.
quinolone
organofluorine compoundAn organofluorine compound is a compound containing at least one carbon-fluorine bond.
primary amino compoundA compound formally derived from ammonia by replacing one hydrogen atom by an organyl group.
secondary amino compoundA compound formally derived from ammonia by replacing two hydrogen atoms by organyl groups.
tertiary amino compoundA compound formally derived from ammonia by replacing three hydrogen atoms by organyl groups.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (1)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Forkhead box protein O1Homo sapiens (human)IC50 (µMol)0.03300.03302.51655.0000AID1892082
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (39)

Processvia Protein(s)Taxonomy
negative regulation of transcription by RNA polymerase IIForkhead box protein O1Homo sapiens (human)
blood vessel developmentForkhead box protein O1Homo sapiens (human)
temperature homeostasisForkhead box protein O1Homo sapiens (human)
intracellular glucose homeostasisForkhead box protein O1Homo sapiens (human)
protein acetylationForkhead box protein O1Homo sapiens (human)
autophagyForkhead box protein O1Homo sapiens (human)
apoptotic processForkhead box protein O1Homo sapiens (human)
DNA damage responseForkhead box protein O1Homo sapiens (human)
insulin receptor signaling pathwayForkhead box protein O1Homo sapiens (human)
cellular response to starvationForkhead box protein O1Homo sapiens (human)
gene expressionForkhead box protein O1Homo sapiens (human)
positive regulation of autophagyForkhead box protein O1Homo sapiens (human)
cellular response to insulin stimulusForkhead box protein O1Homo sapiens (human)
negative regulation of stress-activated MAPK cascadeForkhead box protein O1Homo sapiens (human)
positive regulation of smooth muscle cell apoptotic processForkhead box protein O1Homo sapiens (human)
cellular response to oxidative stressForkhead box protein O1Homo sapiens (human)
positive regulation of apoptotic processForkhead box protein O1Homo sapiens (human)
negative regulation of apoptotic processForkhead box protein O1Homo sapiens (human)
fat cell differentiationForkhead box protein O1Homo sapiens (human)
negative regulation of fat cell differentiationForkhead box protein O1Homo sapiens (human)
positive regulation of gluconeogenesisForkhead box protein O1Homo sapiens (human)
positive regulation of protein catabolic processForkhead box protein O1Homo sapiens (human)
negative regulation of DNA-templated transcriptionForkhead box protein O1Homo sapiens (human)
positive regulation of DNA-templated transcriptionForkhead box protein O1Homo sapiens (human)
positive regulation of transcription by RNA polymerase IIForkhead box protein O1Homo sapiens (human)
negative regulation of insulin secretionForkhead box protein O1Homo sapiens (human)
canonical Wnt signaling pathwayForkhead box protein O1Homo sapiens (human)
regulation of transcription initiation by RNA polymerase IIForkhead box protein O1Homo sapiens (human)
cellular response to coldForkhead box protein O1Homo sapiens (human)
response to fatty acidForkhead box protein O1Homo sapiens (human)
cellular response to hyperoxiaForkhead box protein O1Homo sapiens (human)
cellular response to nitric oxideForkhead box protein O1Homo sapiens (human)
negative regulation of canonical Wnt signaling pathwayForkhead box protein O1Homo sapiens (human)
energy homeostasisForkhead box protein O1Homo sapiens (human)
neuronal stem cell population maintenanceForkhead box protein O1Homo sapiens (human)
negative regulation of cardiac muscle hypertrophy in response to stressForkhead box protein O1Homo sapiens (human)
regulation of neural precursor cell proliferationForkhead box protein O1Homo sapiens (human)
regulation of reactive oxygen species metabolic processForkhead box protein O1Homo sapiens (human)
regulation of transcription by RNA polymerase IIForkhead box protein O1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (14)

Processvia Protein(s)Taxonomy
DNA-binding transcription factor activity, RNA polymerase II-specificForkhead box protein O1Homo sapiens (human)
DNA-binding transcription repressor activity, RNA polymerase II-specificForkhead box protein O1Homo sapiens (human)
DNA-binding transcription activator activity, RNA polymerase II-specificForkhead box protein O1Homo sapiens (human)
nucleic acid bindingForkhead box protein O1Homo sapiens (human)
chromatin bindingForkhead box protein O1Homo sapiens (human)
DNA-binding transcription factor activityForkhead box protein O1Homo sapiens (human)
protein bindingForkhead box protein O1Homo sapiens (human)
beta-catenin bindingForkhead box protein O1Homo sapiens (human)
chromatin DNA bindingForkhead box protein O1Homo sapiens (human)
ubiquitin protein ligase bindingForkhead box protein O1Homo sapiens (human)
sequence-specific DNA bindingForkhead box protein O1Homo sapiens (human)
protein phosphatase 2A bindingForkhead box protein O1Homo sapiens (human)
promoter-specific chromatin bindingForkhead box protein O1Homo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingForkhead box protein O1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (6)

Processvia Protein(s)Taxonomy
nucleusForkhead box protein O1Homo sapiens (human)
nucleusForkhead box protein O1Homo sapiens (human)
nucleoplasmForkhead box protein O1Homo sapiens (human)
cytoplasmForkhead box protein O1Homo sapiens (human)
mitochondrionForkhead box protein O1Homo sapiens (human)
cytosolForkhead box protein O1Homo sapiens (human)
chromatinForkhead box protein O1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (15)

Assay IDTitleYearJournalArticle
AID1892083Antiproliferative activity against human iPSC derived cardiomyocytes assessed as increase in cell number by measuring fold change after 3 passages at 100 nM incubated for 2 days by Hoechst staining based analysis2022Bioorganic & medicinal chemistry, 07-01, Volume: 65Phenotypic screen identifies FOXO inhibitor to counteract maturation and promote expansion of human iPS cell-derived cardiomyocytes.
AID1892082Inhibition of FOXO-1 in human HepG2 cells incubated for 20 hrs by Renilla luciferase reporter gene assay2022Bioorganic & medicinal chemistry, 07-01, Volume: 65Phenotypic screen identifies FOXO inhibitor to counteract maturation and promote expansion of human iPS cell-derived cardiomyocytes.
AID1892089Downregulation of NPPA gene expression in human iPSC derived cardiomyocytes measured after two passages following incubation for 5 days by qRT PCR analysis2022Bioorganic & medicinal chemistry, 07-01, Volume: 65Phenotypic screen identifies FOXO inhibitor to counteract maturation and promote expansion of human iPS cell-derived cardiomyocytes.
AID1892093Downregulation of MYL2 gene expression in human iPSC derived cardiomyocytes at 100 nM incubated for 5 days by qRT-PCR analysis2022Bioorganic & medicinal chemistry, 07-01, Volume: 65Phenotypic screen identifies FOXO inhibitor to counteract maturation and promote expansion of human iPS cell-derived cardiomyocytes.
AID1892087Downregulation of MYH7 gene expression in human iPSC derived cardiomyocytes measured after two passages following incubation for 5 days by qRT PCR analysis2022Bioorganic & medicinal chemistry, 07-01, Volume: 65Phenotypic screen identifies FOXO inhibitor to counteract maturation and promote expansion of human iPS cell-derived cardiomyocytes.
AID1892091Downregulation of ANP protein level in human iPSC derived cardiomyocytes at 100 nM incubated for 3 weeks by immunofluorescence assay2022Bioorganic & medicinal chemistry, 07-01, Volume: 65Phenotypic screen identifies FOXO inhibitor to counteract maturation and promote expansion of human iPS cell-derived cardiomyocytes.
AID1892084Upregulation of MYH6 gene expression in human iPSC derived cardiomyocytes at 100 nM incubated for 5 days by qRT-PCR analysis2022Bioorganic & medicinal chemistry, 07-01, Volume: 65Phenotypic screen identifies FOXO inhibitor to counteract maturation and promote expansion of human iPS cell-derived cardiomyocytes.
AID1892085Upregulation of TBX2 gene expression in human iPSC derived cardiomyocytes at 100 nM incubated for 5 days by qRT-PCR analysis2022Bioorganic & medicinal chemistry, 07-01, Volume: 65Phenotypic screen identifies FOXO inhibitor to counteract maturation and promote expansion of human iPS cell-derived cardiomyocytes.
AID1892080Antiproliferative activity against human iPSC derived cardiomyocytes assessed as fold increase in cell number at 100 nM incubated for 4 days without passaging by Hoechst staining based analysis2022Bioorganic & medicinal chemistry, 07-01, Volume: 65Phenotypic screen identifies FOXO inhibitor to counteract maturation and promote expansion of human iPS cell-derived cardiomyocytes.
AID1892094Downregulation of NPPA gene expression in human iPSC derived cardiomyocytes at 100 nM incubated for 5 days by qRT-PCR analysis2022Bioorganic & medicinal chemistry, 07-01, Volume: 65Phenotypic screen identifies FOXO inhibitor to counteract maturation and promote expansion of human iPS cell-derived cardiomyocytes.
AID1892090Downregulation of MLC2v protein level in human iPSC derived cardiomyocytes at 100 nM incubated for 3 weeks by immunofluorescence assay2022Bioorganic & medicinal chemistry, 07-01, Volume: 65Phenotypic screen identifies FOXO inhibitor to counteract maturation and promote expansion of human iPS cell-derived cardiomyocytes.
AID1892088Downregulation of MYL2 gene expression in human iPSC derived cardiomyocytes measured after two passages following incubation for 5 days by qRT PCR analysis2022Bioorganic & medicinal chemistry, 07-01, Volume: 65Phenotypic screen identifies FOXO inhibitor to counteract maturation and promote expansion of human iPS cell-derived cardiomyocytes.
AID1892092Downregulation of MYH7 gene expression in human iPSC derived cardiomyocytes at 100 nM incubated for 5 days by qRT-PCR analysis2022Bioorganic & medicinal chemistry, 07-01, Volume: 65Phenotypic screen identifies FOXO inhibitor to counteract maturation and promote expansion of human iPS cell-derived cardiomyocytes.
AID1892081Cytotoxicity against human iPSC derived cardiomyocytes at >=500 nM incubated for 4 days without passaging by Hoechst staining based analysis2022Bioorganic & medicinal chemistry, 07-01, Volume: 65Phenotypic screen identifies FOXO inhibitor to counteract maturation and promote expansion of human iPS cell-derived cardiomyocytes.
AID1892086Upregulation of IRX4 gene expression in human iPSC derived cardiomyocytes aat 100 nM incubated for 5 days by qRT-PCR analysis2022Bioorganic & medicinal chemistry, 07-01, Volume: 65Phenotypic screen identifies FOXO inhibitor to counteract maturation and promote expansion of human iPS cell-derived cardiomyocytes.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (35)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's22 (62.86)24.3611
2020's13 (37.14)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 12.93

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be weak demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index12.93 (24.57)
Research Supply Index3.58 (2.92)
Research Growth Index6.52 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (12.93)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews2 (5.71%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other33 (94.29%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]